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    • 105. 发明申请
    • NOVEL BORNEOL DERIVATIVES, METHODS OF MANUFACTURING THEM, AND THEIR PHARMACEUTICAL USE
    • 新BORNEOLDERIVATE,PROCESS FOR THEIR和制药用
    • WO1996025392A1
    • 1996-08-22
    • PCT/DE1996000297
    • 1996-02-19
    • SCHERING AKTIENGESELLSCHAFTKLAR, UlrichGRAF, HermannNEEF, GünterBLECHERT, Siegfried
    • SCHERING AKTIENGESELLSCHAFT
    • C07C271/22
    • C07D303/16C07C271/22C07C2603/86
    • The invention concerns borneol derivatives of general formula (I), wherein: R represents C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NH(C(O)-CH(OR )-CH(NR R )-R )] -R ; R and R are identical or different and the same as R ; R and R are identical or different and the same as R ; R is -C(O)R , -SO2R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , (a), alkyl; R is phenyl; R and R are identical or different and stand for alkyl, cycloalkyl, aryl or aralkyl; R are identical or different and stand for hydrogen, alkyl, aryl, acyl, aralkyl, -SO2R , -P(O) (OH)2; R stands for hydrogen, alkyl, aryl, aralkyl. The invention also concerns salts of the said compounds with physiologically tolerable bases, alpha -, beta - or gamma -cyclodextrine clathrates of the said compounds and compounds of formula (I) encapsulated with liposomes. The compounds are active as tubulin polymerisation antagonists.
    • 本发明betrfifft Borneolderivate通式(I)其中R <1>(O)-CH(OR <6>)C - CH(NR <7A> - [R <7B>) - R的<8>,C(O) -CH(OR <6>) - CH [NH((O)-CH(OR <6B>)C - CH(NR <7A> - [R <7B>) - R的<8>)] - R的<8>, [R <6A>,R <6B>是相同的或不同的并且R <6>,R <7A>,R <7B>是相同的或不同的并且R <7>,R <7> -C(O)R <12>,-SO 2 R <12>,-C(O)OR <12>,-C(O)SR <12>,-C(O)NHR <9D>,-C(O)NR <9D>ř <9A>中,(a)烷基,R <8>是苯基,R ,R <12>是相同的或不同的并且是烷基,环烷基,芳基,芳烷基,R <6>是相同的或不同的,是氢 烷基,芳基,酰基,芳烷基,-SO 2 R <9C>,-P(O)(OH)指2,R <13>为氢,烷基,芳基,芳烷基,以及与生理上可耐受的碱,以及它们的α它们的盐 - ,β - 或伽马-Cyclodextrinclathrate和平均封装有通式(I)的脂质体的化合物。 该化合物作为活性聚合的微管蛋白拮抗剂。
    • 109. 发明申请
    • PROCESS FOR FILLING WITH A FLUID AND CLOSING DISPOSABLE SYRINGES THAT ARE TO BE STERILISED
    • 填充和与FLUIDEM目录合闸方式,需要消毒的一次性注射器
    • WO1996013289A2
    • 1996-05-09
    • PCT/DE1995001523
    • 1995-10-27
    • SCHERING AKTIENGESELLSCHAFTSPECK, Ulrich
    • SCHERING AKTIENGESELLSCHAFT
    • A61M05/28
    • A61M5/34A61M5/001A61M5/1782A61M5/28A61M5/3134A61M5/315A61M5/31505A61M5/32A61M2005/3104A61M2005/3118A61M2005/3139A61M2005/3279A61M2207/00B65B3/003
    • A process is disclosed for filling with a fluid and closing disposable plastic syringes that are to be sterilised. The disposable syringes have an injection cylinder (11) with a shaped front nozzle part (20), a piston or piston plug (30) in at least one piece and a piston stop element (40) arranged in the area of the cylinder gripping plate (12). After inserting the piston (30) into the empty injection cylinder (11), together or not with its own piston rod, the piston is fully pushed up to the front end of the cylinder. The fluid medium is then fed under pressure into the injection cylinder (11) through the nozzle part (20) and pushes the piston (30) in the direction of the piston rod up to the piston stop element (40). After the syringe is filled, the front area (25) of the nozzle part (20) is closed by plastic deformation. This process allows a previously filled disposable syringe to be sterilised in a standard autoclave without any risk of the syringe inner pressure plastically deforming parts of the syringe.
    • 本发明涉及一种用于填充密封一个与fluidem内容的方法来进行灭菌由塑料制成的,一次性注射器,其中所述一次性注射器注射器筒(11),其具有前整体形成的喷嘴部分(20),一个至少单件式活塞或柱塞止动件(30)和一个在所述范围内 气缸把手板(12)位于活塞止挡元件(40)。 所述活塞(30)被完全插入时,插入空的注射器筒(11)具有或不具有其自己的活塞杆到其前端之后。 随后,经由注射器筒(11)在喷嘴部(20)压力下的流体介质被按压,其中,所述流体介质推动活塞(30)朝向所述活塞杆侧到活塞止挡元件(40)向前。 填充喷嘴部分的前部(25)后(20)由塑性变形封闭。 使用本发明的方法中,预填充的一次性注射器可在Standardautoklaven进行灭菌而不会由于内压注射器针筒部件有的塑性变形的危险。